GSK-J4, H3K27 Histone Demethylases UTX and JMJD3 Inhibitor


Catalog No. size PriceQuantity
M60063-2D 2 mg in DSMO (0.479 mL) $113
M60063-2S 2mg solid $114
M60063-10S 10mg solid $447

Description

Product Information
Molecular Weight: 417.50
Formula: C24H27N5O2
Purity: ≥98%
CAS#: 1373423-53-0
Solubility: DMSO up to 100 mM
Chemical Name: ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

GSK-J4 is an ethyl ester derivative of GSK-J1, which is the first selective and potent inhibitor of the H3K27 histone demethylases UTX and JMJD3. The highly polar carboxylate group of GSK-J1 restricts its cellular permeability, therefore GSK-J4 was developed as a pro-drug, masking the polarity of the acid group of the GSK-J1, for cellular assays. GSK-J4 could significant reduce LPS-induced pro-inflammatory cytokine production in primary human macrophages (IC50 ~9 μM for the inhibition of TNFα release). Together with GSK-J1, GSK-J4 could be a unique small molecule to allow selective pharmacological intervention across the JMJ family.

 

How to Use:

 

  • In vitro:  GSK-J4 was used at 30 µM final concentration in cellular assays.
  • In vivo: n/a

 

 

Reference:

  • 1. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response (2012) Nature. 488(7411):404-8.
  • 2. SGC website: http://www.thesgc.org/scientists/chemical_probes/GSKJ1 

 

Products are for research use only. Not for human use. 

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